| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H16ClF2N5O2 |
| Molecular Weight | 431.823 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](N1C=NC2=CC(Cl)=CC=C2C1=O)[C@](O)(CN3C=NC=N3)C4=CC=C(F)C=C4F
InChI
InChIKey=UHIXWHUVLCAJQL-MPBGBICISA-N
InChI=1S/C20H16ClF2N5O2/c1-12(28-11-25-18-6-13(21)2-4-15(18)19(28)29)20(30,8-27-10-24-9-26-27)16-5-3-14(22)7-17(16)23/h2-7,9-12,30H,8H2,1H3/t12-,20-/m1/s1
| Molecular Formula | C20H16ClF2N5O2 |
| Molecular Weight | 431.823 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Albaconazole is a triazole antifungal. Azoles are important antifungal compounds, and all drugs in this class inhibit ergosterol synthesis by blocking the 14-α-demethylase enzyme, resulting in the accumulation of toxic methylsterols that may culminate in fungal death. Albaconazole, an oral agent that has demonstrated high levels of bioavailability and potent antifungal activity. It was under development for the treatment of onychomycosis, vulvovaginal candidiasis. Also, albaconazole was evaluated in phase I, a randomized, placebo-controlled clinical trial in patients with tinea pedis. No serious adverse effects occurred in the studies involving albaconazole. However, this researches on this drug were discontinued.
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The clinically relevant intracellular amastigote forms, proliferating in cultured Vero cells at 37°C, were more susceptible to Albaconazole than epimastigotes: the MIC required to reduce infected cells by 99% and the IC50 (concentration of the drug required to reduce infected cells by 50%) were in this case 10 nM and 1 nM, respectively.
